兰索拉唑在胃溃疡患者及健康人体内的药动学研究

Pharmacokinetic Study of Lansoprazole in Gastric Ulcer Patients and Healthy Volunteers

目的:比较兰索拉唑在胃溃疡患者及健康人体内药动学行为的差异。方法:12名男性受试者(健康者和胃溃疡患者各6名),静脉滴注300mg·L-1兰索拉唑注射液250mL后于不同时间点取血并分离血浆,采用高效液相色谱-二极管阵列检测器(HPLC-DAD)法检测血浆中兰索拉唑的浓度,以DAS2.0软件计算药动学参数。结果:健康者与胃溃疡患者静脉给予兰索拉唑后,人体内药动学参数分别为:t1/(22.369±1.51)、(2.835±0.99)h,tma(x0.332±0.09)、(0.277±0.05)h,CL(19.882±8.19)、(14.460±7.79)L·h-1,cma(x1092.09±169.69)、(910.76±69.91)ng·mL-1,AUC0～6.(51475.98±590.23)、(2278.73±567.92)ng·h·mL-1,MRT0～6.(51.633±0.44)、(1.833±0.42)h。结论:兰索拉唑在胃溃疡患者体内的药动学过程较健康者发生了显著变化。

OBJECTIVE：To compare the differences of pharmacokinetic profiles of lansoprazole between gastric ulcer patients and healthy volunteers in vivo.METHODS：12 male subjects （6 gastric ulcer patients and 6 healthy volunteers） were given Lansoprazole injection 250 mL via intravenous drip,and then the blood samples were collected at different time points.The concentration of lansoprazole was determined by HPLC-DAD.The pharmacokinetic parameters were analyzed using DAS2.0 software.RESULTS：The pharmacokinetic parameters of lansoprazole in healthy volunteers vs.gastric ulcer patients after intravenous administration were as follows：t1/2（2.369±1.51）h vs.（2.835±0.99）h,tmax（0.332±0.09） h vs.（0.277±0.05）h,CL（19.882±8.19）L·h-1 vs.（14.460±7.79） L·h-1,cmax（1 092.09±169.69） μg·L-1 vs.（910.76±69.91）ng·mL-1,AUC0～6.5（1 475.98±590.23）ng·h·mL-1 vs.（2 278.73±567.92）ng·h·mL-1,MRT0～6.5（1.633±0.44）h vs.（1.833±0.42）h.CONCLUSION：The pharmacokinetic profiles of lansoprazole in gastric ulcer patients have changed compared with healthy volunteers.